上海交通大学学报（医学版）

上海交通大学学报（医学版） ›› 2018, Vol. 38 ›› Issue (3): 339-.doi: 10.3969/j.issn.1674-8115.2018.03.018

• 综述 • 上一篇    下一篇

前蛋白转化酶枯草溶菌素 9 单克隆抗体治疗冠状动脉粥样硬化性心脏病的临床研究进展

罗聪聪 1 ，鲍春荣 2 ，何斌 1   

  1. 上海交通大学 医学院附属新华医院 1. 麻醉与重症医学科，2. 心胸外科，上海 200092
  • 出版日期:2018-03-28 发布日期:2018-05-03
  • 通讯作者: ?何 斌，电子信箱：hebinicu@xinhuamed.com.cn。
  • 作者简介:?罗聪聪（1992—），男，壮族，硕士生；电子信箱：luocongcong1@163.com。
  • 基金资助:
    国家自然科学基金（81470390）；上海市教育委员会高峰高原学科建设计划（20152218）；上海交通大学医工交叉项目（YG2013MS21）

Clinical advances in monoclonal antibody against PCSK9 for coronary atherosclerotic heart disease

LUO Cong-cong1 , BAO Chun-rong2 , HE Bin1   

  1. 1. Department of Anesthesiology and SICU, 2. Department of Cardiothoracic Surgery, Xinhua Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200092, China
  • Online:2018-03-28 Published:2018-05-03
  • Supported by:
    Natural Science Foundation of China, 81470390; Shanghai Municipal Education Commission—Gaofeng Clinical Medicine Grant Support, 20152218; Biomedical Engineering Cross Research Foundation of Shanghai Jiao Tong University, YG2013MS21

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摘要： 冠状动脉粥样硬化性心脏病（coronary atherosclerotic heart disease，CHD）的发病率及病死率居全球首位，而低密度脂蛋白胆固醇（low density lipoprotein-cholesterol，LDL-C）的升高是 CHD 的主要危险因素，因此降低 LDL-C 水平可有效减少 CHD 的发病风险。临床上降脂药物如他汀类虽能够有效降低 LDL-C 水平，但仍有部分患者无法达到降脂目标或者无法耐受。前蛋白转化酶枯草溶菌素 9（proprotein convertase subtilisin/kexin type 9，PCSK9）抑制剂作为新一代的降脂药物，越来越受到重视。其通过对 PCSK9 的抑制作用，增加低密度脂蛋白受体的循环利用，能够显著降低血清中 LDL-C 水平。目前 PCSK9 抑制剂已进入Ⅲ期临床试验，试验结果显示其具有良好的降脂效果和耐受性。该文就 PCSK9 抑制剂最新进展和面临的问题作一综述。

关键词: &ensp, 前蛋白转化酶枯草溶菌素 9；抑制剂；单克隆抗体；低密度脂蛋白胆固醇；冠状动脉粥样硬化性心脏病；高脂血症

Abstract:

Coronary atherosclerotic heart disease (CHD) remains the leading cause of morbidity and mortality in the world, with elevated low density lipoprotein-cholesterol (LDL-C) levels as a major risk factor. Lower levels of LDL-C can effectively reduce the risk of CHD. To date, lipid-lowering medicines such as statins are effective in lowering LDL-C, but a proportion of patients do not achieve lipid reduction target with statins or are intolerant to statins. Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors are a new class of agents reducing LDL-C which gain more and more concerns. Through inhibitory effect on PCSK9 and increasing low-density lipoprotein receptors recycling, they can significantly reduce serum LDL-C levels. PCSK9 inhibitors are currently in phase Ⅲ of clinical trials, and the results showed that they had good lipid-lowering effects and tolerability. This review provided an overview of the latest advances and challenges about PCSK9 inhibitors.

Key words: proprotein convertase subtilisin/kexin type 9 (PCSK9), inhibitor, monoclonal antibody, low-density lipoprotein-cholesterol (LDL-C), coronary atherosclerotic heart disease (CHD), hyperlipidemia